Assay Detail
Functional
CHEMBL754271
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Opioid receptor kappa 1 as reduced contraction in electrically stimulated rabbit vas deferens
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
trans N-Methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] cycloprop-2-ene-1-carboxamides: Novel lipophilic kappa opioid agonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 7.22 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL318859 | ENADOLINE | 2.0 | 1 | 8.48 |
| CHEMBL102040 | — | — | 1 | 8.02 |
| CHEMBL98893 | — | — | 1 | 7.66 |
| CHEMBL317102 | — | — | 1 | 7.50 |
| CHEMBL100994 | — | — | 1 | 6.85 |
| CHEMBL318215 | — | — | 1 | 6.52 |
| CHEMBL329755 | — | — | 1 | 5.52 |
| CHEMBL317179 | — | — | 1 | - |
| CHEMBL319768 | — | — | 1 | - |
| CHEMBL327944 | — | — | 1 | - |
| CHEMBL101604 | — | — | 1 | - |
| CHEMBL318430 | — | — | 1 | - |
| CHEMBL318034 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL318859 | ENADOLINE | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL102040 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL98893 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL317102 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL100994 | — | EC50 | = | 141.0 | nM | 6.85 |
| CHEMBL318215 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL329755 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL317179 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL319768 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL327944 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL101604 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL318430 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL318034 | — | EC50 | > | 10000.0 | nM | - |